Elvitegravir-GS-9137-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEElvitegravirCat. No.: HY-14740CAS No.: 697761-98-1Synonyms: GS-9137; JTK-303; D06677分式: CHClFNO分量: 447.88作靶點(diǎn): HIV Integrase; HIV作通路: Metabolic Enzyme/Protease; Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mo

2、nths-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (111.64 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.58 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.58 mM); Suspended solution; Need ultra

3、sonic3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.58 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Elvitegravir種 HIV integrase 抑制劑，作于 HIV-1IIIB，HIV-2EHO 和 HIV-2ROD，IC50 分別為 0.7nM，2.8 nM 和 1.4 nM。IC50 & Target IC50: 0.7 nM (HIV-1IIIB), 2.8 nM (HIV-2EHO), 1.4 nM(HIV-2ROD) 1體外研究 Elvitegravir

4、 (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer.Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinicalisolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus

5、(MLV) andsimian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratorystrains of HIV, with EC50 values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir isevaluated against wild-type clinical isolates representing various subtypes

6、 of HIV-1. Elvitegravir suppressesthe replication of all HIV-1 subtypes tested, with an antiviral EC50 ranging from 0.1 to 1.26 nM. Moreover,Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor,

7、 the compound L-870,810. The cytotoxicities of theseinhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration thatsuppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from threeindependent donors are 4.60.5 M and 2.70

8、.6 M, respectively. Thus, Elvitegravir can suppress variousHIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated withresistance to currently approved antiretroviral drugs 1.PROTOCOLCell Assay 1 MT-2 cells (2105 cells) are infected with HIV-1 IIIB

9、and then cultured in the presence of 0.5 nM or 0.1 nMElvitegravir. Cultures are incubated at 37C until an extensive cytopathic effect (CPE) is observed, and theculture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration ofElvitegravir is increased when a signific

10、ant CPE is observed. At the indicated passages, proviral DNA isextracted from infected MT-2 cells and then subjected to PCR, followed by direct population-basedsequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay orp24 production 1.MCE has not indep

11、endently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Physiol Biochem. 2016;38(3):1111-20. Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670. Antiviral Res. 2019 Feb;162:101-109.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE J Neuroimmune Pharmacol. 2

12、019 Jul 23. Toxicol Appl Pharmacol. 2019 Apr 1;368:18-25.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Shimura K, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitorelvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74.McePdfHeightCaution: